专利号:US-11325888-B2 优先权日:2017-08-11 标 题:Method for the synthesis of monoprotected bifunctional prodrugs and antibody drug conjugates based thereon as well as a method for preparing antibody drug conjugates 发明人:TIETZE LUTZ F 权利人:GEORG AUGUST UNIV GOETTINGEN STIFTUNG OEFFENTLICHEN RECHTS 摘要:The present invention relates to a method for the synthesis of compounds useful in the preparation of antibody drug conjugates (ADC), namely, monoprotected dimeric bifunctional prodrugs based on duocarmycin analogs. In a further aspect, compounds obtained by the method according to the present invention are provided. The monoprotected bifunctional prodrug is used for preparing antibody drug conjugates composed of an antibody moiety and the monoprotected bifunctional prodrug. The antibody compound conjugates thus obtained are provided. Further, a method of preparing an antibody drug conjugate composed of two identical or two different antibody moieties is provided as well as the antibody compound conjugate containing two different antibody moieties accordingly. These conjugates can be used in pharmaceutical compositions, in particular, for use in treatment of tumors, e.g. for use in ADC therapy.
专利号:US-5194562-A 优先权日:1989-02-22 标题:Nucleophilic displacement method for synthesis of non-rigid PBZ polymers 发明人:INBASEKARAN MUTHIAH N; MULLINS MICHAEL J 权利人:DOW CHEMICAL CO 摘要:Azole rings, such as oxazole and thiazole rings, can activate an aromatic ring bonded to a leaving group such as a halogen atom so that the aromatic ring will undergo aromatic nucleophilic substitution. The reaction is useful for making ethers, thioethers and amines containing azole rings. In particular, monomers having azole rings, activated aromatic rings with leaving groups and nucleophilic moieties can react under conditions of aromatic nucleophilic displacement to form non-rigid rob PBZ polymers. The non-rigid rod PBZ polymers can be used to form molecular composites with rigid rod PBZ polymers which molecular composites are not substantially phase separated.
专利号:US-5216110-A 优先权日:1989-02-22 标题 :Monomers useful in nucleophilic displacement synthesis of polybenzazole polymers 发明人:INBASEKARAN MUTHIAH N; MULLINS MICHAEL J 权利人:DOW CHEMICAL CO 摘要:Azole rings, such as oxazole and thiazole rings, can activate an aromatic ring bonded to a leaving group such as a halogen atom so that the aromatic ring will undergo aromatic nucleophilic substitution. The reaction is useful for making ethers, thioethers and amines containing azole rings. In particular, monomers having azole rings, activated aromatic rings with leaving groups and nucleophilic moieties can react under conditions of aromatic nucleophilic displacement to form non-rigid rod PBZ polymers. The non-rigid rod PBZ polymers can be used to form molecular composites with rigid rod PBZ polymers which molecular composites are not substantially phase separated.
专利号:US-5104960-A 优先权日:1989-02-22 标 题:Nucleophilic displacement method for synthesis of non-rigid PBZ polymers 发明人:INBASEKARAN MUTHIAH N; MULLINS MICHAEL J 权利人:DOW CHEMICAL CO 摘要:Azole rings, such as oxazole and thiazole rings, can activate an aromatic ring bonded to a leaving group such as a halogen atom so that the aromatic ring will undergo aromatic nucleophilic substitution. The reaction is useful for making ethers, thioethers and amines containing azole rings. In particular, monomers having azole rings, activated aromatic rings with leaving groups and nucleophilic moieties can react under conditions of aromatic nucleophilic displacement to form non-rigid rod PBZ polymers. The non-rigid rod PBZ polymers can be used to form molecular composites with rigid rod PBZ polymers which molecular composites are not substantially phase separated.
专利号:US-7202030-B2 优先权日:2001-11-01 标 题:Solid-phase array-based biocatalytic transformations 发明人:DORDICK JONATHAN S; SANTHANAM LAKSHMI; HOGG MICHAEL G; HOLLAND JAMES A 权利人:US SECRETARY DEPT OF VETERANS 摘要:This invention relates to the enzymatic synthesis of oligophenols on solid support by sequential enzymatic addition of reaction solutions containing phenols. The oligomers are then selectively built up on the solid surface. When used in a specific format, the oligomers can be generated in a spatially addressable array, which can then be screened for some type of biological interaction. The synthetic compounds of the present invention are synthesized in a combinatorial manner on solid support using peroxidase or other related enzymatic catalysis, and the products are generated in spatially addressable microarrays. Oligophenols of the present invention have shown significance as potential inhibitors of NADPH oxidase assembly, an enzyme that has been implicated in a wide range of diseases stemming from vascular hyperpermeability.
专利号:WO-2024114106-A1 优先权日:2022-11-29 标 题:Sulfentrazone intermediate synthesis method 发明人:LI ZHIQING; XIE YONGKANG; ZHAO GUANGLI; LIU QIANG; XU YANLEI; LI HAIHUA 权利人:NINGXIA RAINBOW CHEMICAL CO LTD 摘要:The present application discloses a sulfentrazone intermediate synthesis method. By adding a composite catalyst, a compound as shown in formula II is subjected to a chlorination reaction in the presence of a solvent to synthesize a compound as shown in formula I. The composite catalyst comprises a catalyst A and a catalyst B at a weight ratio of 0.1-20: 0.01-10; the catalyst A is one or more of a metal or metal chloride; and the catalyst B is a compound capable of reacting with water to remove water in a reaction system. The method of the present application is simple to operate and easy to industrialize, the reaction environment is relatively mild, the used catalyst is cheap and easy to obtain, and the reaction yield and the product content are high.